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Pracinostat (dihydrochloride)

Pracinostat dihydrochloride is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research. Pracinostat dihydrochloride also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM[1][4].

Product Specifications

CAS Number

929016-98-8

UNSPSC

12352005

Target

Apoptosis; Beta-lactamase; HDAC

Type

Reference compound

Related Pathways

Anti-infection; Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pracinostat-dihydrochloride.html

Solubility

10 mM in DMSO

Smiles

CCN(CCN1C2=CC=C(C=C2N=C1CCCC)/C=C/C(NO)=O)CC.Cl.Cl

Molecular Formula

C20H32Cl2N4O2

Molecular Weight

431.40

References & Citations

[1]Novotny-Diermayr V, et al. SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer. Mol Cancer Ther. 2010 Mar;9 (3) :642-52.|[2]Wang H, et al. Discovery of (2E) -3-{2-butyl-1-[2- (diethylamino) ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. J Med Chem. 2011 Jul 14;54 (13) :4694-720.|[3]Novotny-Diermayr V, et al. The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML. Blood Cancer J. 2012 May;2 (5) :e69.|[4]Lechner S, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Aug;18 (8) :812-820.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Launched

Frequently Asked Questions

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